Target
Cyclin-dependent kinase 5 activator 1 [99-307]
Ligand
BDBM7265
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
60±n/a nM
Comments
extracted
Citation
 Leost, MSchultz, CLink, AWu, YZBiernat, JMandelkow, EMBibb, JASnyder, GLGreengard, PZaharevitz, DWGussio, RSenderowicz, AMSausville, EAKunick, CMeijer, L Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem 267:5983-94 (2000) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 5 activator 1 [99-307]
Synonyms:
CDK5/p25 | Cyclin-Dependent Kinase 5 (CDK5)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-dependent kinase 5
Synonyms:
CDK5 | CDK5_HUMAN | CDKN5 | Cell division protein kinase 5 | Cyclin-dependent kinase 5 (CDK5/ p25) | Cyclin-dependent kinase 5 (CDK5/p35) | Cyclin-dependent-like kinase 5 | Cyclin-dependent-like kinase 5 (CDK5) | PSSALRE | Serine/threonine-protein kinase PSSALRE | Tau protein kinase II catalytic subunit
Type:
Enzyme Subunit
Mol. Mass.:
33308.61
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
292
Sequence:
MQKYEKLEKIGEGTYGTVFKAKNRETHEIVALKRVRLDDDDEGVPSSALREICLLKELKHKNIVRLHDVLHSDKKLTLVFEFCDQDLKKYFDSCNGDLDPEIVKSFLFQLLKGLGFCHSRNVLHRDLKPQNLLINRNGELKLADFGLARAFGIPVRCYSAEVVTLWYRPPDVLFGAKLYSTSIDMWSAGCIFAELANAGRPLFPGNDVDDQLKRIFRLLGTPTEEQWPSMTKLPDYKPYPMYPATTSLVNVVPKLNATGRDLLQNLLKCNPVQRISAEEALQHPYFSDFCPP
  
Component 2
Name:
Cyclin-dependent kinase 5 activator 1 [99-307]
Synonyms:
CD5R1_HUMAN | CDK5R | CDK5R1 | Cyclin-Dependent Kinase 5 Activator | Cyclin-dependent kinase 5 activator 1, p25 | NCK5A | TPKII regulatory subunit | p25
Type:
Enzyme Subunit
Mol. Mass.:
23250.56
Organism:
Homo sapiens (Human)
Description:
Q15078 aa 99-307
Residue:
209
Sequence:
AQPPPAQPPAPPASQLSGSQTGGSSSVKKAPHPAVTSAGTPKRVIVQASTSELLRCLGEFLCRRCYRLKHLSPTDPVLWLRSVDRSLLLQGWQDQGFITPANVVFLYMLCRDVISSEVGSDHELQAVLLTCLYLSYSYMGNEISYPLKPFLVESCKEAFWDRCLSVINLMSSKMLQINADPHYFTQVFSDLKNESGQEDKKRLLLGLDR
  
Inhibitor
Name:
BDBM7265
Synonyms:
4,5-dimethoxy-9-oxo-8,18-diazatetracyclo[9.7.0.0^{2,7}.0^{12,17}]octadeca-1(11),2,4,6,12(17),13,15-heptaene-14-carbonitrile | 9-cyano-2,3-dimethoxypaullone | NSC 708244 | Paullone Analog 4
Type:
Small organic molecule
Emp. Form.:
C19H15N3O3
Mol. Mass.:
333.3407
SMILES:
COc1cc2NC(=O)Cc3c([nH]c4ccc(cc34)C#N)-c2cc1OC
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
n/a
Residue:
3
Sequence:
NA